专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO1992011267A1 NOVEL METHYLENEBISPHOSPHONIC ACID DERIVATIVES 审中-公开
标题翻译：新型亚甲基双膦酸衍生物
公开(公告)号：WO1992011267A1
公开(公告)日：1992-07-09
申请号：PCT/FI1991000394
申请日：1991-12-18
申请人： HUHTAMÄKI OY , NIKANDER, Hannu , HEIKKILÄ-HOIKKA, Marjaana , POHJALA, Esko , HANHIJÄRVI, Hannu , LAUREN, Leena
发明人： HUHTAMÄKI OY
IPC分类号： C07F09/40
CPC分类号： C07F9/5537 , C07F9/4025
摘要： Novel pharmacologically active methylenebisphosphonates having formula (I) wherein R , R , R and R independently are straight or branched, optionally unsaturated C1-C10-alkyl, optionally unsaturated C3-C10-cycloalkyl, aryl, aralkyl, silyl SiR3 or hydrogen, whereby in formula (I) at least one of the groups R , R , R and R is hydrogen and at least one of the groups is different from hydrogen, Q is hydrogen, hydroxyl, halogen, amino NH2, or OR', wherein R' is C1-C4-lower alkyl or acyl, Q is straight or branched, optionally unsaturated C1-C10-alkyl, -hydroxyalkyl or -aminoalkyl, whereby the oxygen may, as a substituent, contain one group or the nitrogen as a substituent may contain one or two groups, which are C1-C4-lower alkyl or acyl, or the two substituents of the nitrogen form together with the nitrogen atom a saturated, partly saturated or an aromatic heterocyclic ring, or Q is optionally substituted and optionally unsaturated C3-C10-cycloalkyl, which optionally is bound to the molecule over a straight or branched alkylene group containing 1-4 C-atoms, including the stereoisomers, such as the geometrical isomers and the optically active isomers, of the compounds, as well as the pharmacologically acceptable salts of these compounds.
摘要翻译：具有式（I）的新的药理活性亚甲基二膦酸酯，其中R 1，R 2，R 3和R 4独立地是直链或支链的，任选不饱和的C 1 -C 10 - 烷基，任选不饱和的C 3 -C 10 - 环烷基，芳基，芳烷基，甲硅烷基SiR 3或氢，其中在式（I）中，基团R 1，R 2，R 3和R 4中的至少一个是氢和至少一个基团不同于氢，Q 1是氢，羟基，卤素，氨基NH 2或OR'，其中R'是C 1 -C 4 - 低级烷基或酰基，Q 2是直链或支链的，任选不饱和的C1-C10 - 烷基， - 羟烷基或 - 氨基烷基，其中氧可以作为取代基含有一个基团，或者氮作为取代基可以含有一个或两个基团，它们是C 1 -C 4 - 低级烷基或酰基，或两个取代基氮原子与氮原子一起饱和，部分饱和或芳族杂环，或Q 2是任选取代的和任选不饱和的C 3 -C 10 - 环烷基，其优选在包含1-4个C原子的直链或支链亚烷基上，包括立体异构体，如化合物的几何异构体和旋光异构体，以及这些化合物的药理学上可接受的盐。

2. 发明申请

WO1990015806A1 NOVEL METHYLENEBISPHOSPHONIC ACID DERIVATIVES 审中-公开
标题翻译：新型亚甲基双膦酸衍生物
公开(公告)号：WO1990015806A1
公开(公告)日：1990-12-27
申请号：PCT/FI1990000163
申请日：1990-06-19
申请人： HUHTAMÄKI OY , POHJALA, Esko , NUPPONEN, Heikki , VEPSÄLÄINEN, Jouko
发明人： HUHTAMÄKI OY
IPC分类号： C07F0
CPC分类号： C07F9/4037 , C07F9/4081
摘要： Novel pharmaceutically active bisphosphonic acid derivatives of formula (I), in which R , R , R and R independently are C1-C22-alkyl, C2-C22-alkenyl, C2-C22-alkynyl, C3-C10-cycloalkyl, C3-C10-cycloalkenyl, aryl, aralkyl, silyl or hydrogen, whereby in the formula (I) at least one of the groups R , R , R and R is hydrogen and at least one of the groups R , R , R and R is different from hydrogen, Q is hydrogen, fluorine, chlorine, bromine or iodine, and Q is chlorine, bromine or iodine, including the stereoisomers, such as the geometrical isomers and optically active isomers, of the compounds, as well as the pharmaceutically acceptable salts of the compounds.
摘要翻译：式（I）的新型药物活性双膦酸衍生物，其中R 1，R 2，R 3和R 4独立地是C 1 -C 22 - 烷基，C 2 -C 22 - 烯基，C 2 -C 22 - 炔基，C 3 -C 10 - 环烷基，C 3 -C 10 - 环烯基，芳基，芳烷基，甲硅烷基或氢，由此在式（I）中R 1，R 2，R 3，且R 4为氢，R 1，R 2，R 3和R 4基团中的至少一个不同于氢，Q 1为氢，氟，氯，溴或碘，Q 2是氯，溴或碘，包括化合物的立体异构体，如几何异构体和旋光异构体，以及化合物的药学上可接受的盐。

3. 发明申请

WO1995026711A1 OPHTHALMIC COMPOSITION WITH DECREASED VISCOSITY 审中-公开
标题翻译：具有降低粘度的眼底组合物
公开(公告)号：WO1995026711A1
公开(公告)日：1995-10-12
申请号：PCT/FI1995000166
申请日：1995-03-29
申请人： LEIRAS OY , REUNAMÄKI, Timo , LEHMUSSAARI, Kari , VARTIAINEN, Eija , OKSALA, Olli , ALARANTA, Sakari , POHJALA, ESKO
发明人： LEIRAS OY
IPC分类号： A61K09/00
CPC分类号： A61K9/0048 , Y10S514/912
摘要： The present invention is directed to an ophthalmic composition in the form of a topical aqueous solution consisting essentially of: an ophthalmologically active agent, an ion sensitive, hydrophilic polymer in an amount of 0.004 to 1.5 % by weight, at least one salt selected from the group of inorganic salts and buffers in a total amount of from 0.01 to 2.0 % by weight, a wetting agent in an amount of 0 to 3.0 % by weight, a preservative in an amount of 0 to 0.02 % by weight, water, and optionally a pH regulating agent in an amount sufficient to give a pH of 4.0 to 8.0 to the composition, the ratio between salt and polymer components being such that the solution exhibits a viscosity of less than 1000 mPas. The composition contains a sufficient amount of polymer to provide for a controlled absorption of the drug into the eye, its viscosity having been reduced to provide for better handling characteristics.
摘要翻译：本发明涉及一种局部水溶液形式的眼用组合物，其基本上由以下组成：眼科活性剂，0.004至1.5重量％的离子敏感性亲水性聚合物，至少一种选自组合的无机盐和缓冲剂的总量为0.01-2.0重量％，润湿剂的量为0-3.0重量％，防腐剂的量为0至0.02重量％，水和任选地一种pH调节剂，其量足以使组合物的pH为4.0-8.0，盐和聚合物组分之间的比例使溶液的粘度小于1000mPa·s。组合物含有足够量的聚合物以提供药物对眼睛的受控吸收，其粘度已经降低以提供更好的处理特性。

4. 发明申请

WO1993024466A1 NOVEL PILOCARPINE DERIVATIVES AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：新型吡啶衍生物及其制备方法
公开(公告)号：WO1993024466A1
公开(公告)日：1993-12-09
申请号：PCT/FI1993000226
申请日：1993-05-26
申请人： LEIRAS OY , JÄRVINEN, Tomi , PEURA, Pekka , SUHONEN, Pekka , URTTI, Arto , HANHIJÄRVI, Hannu , POHJALA, Esko
发明人： LEIRAS OY
IPC分类号： C07D233/64
CPC分类号： C07D233/64
摘要： The object of the invention are pharmaceutically useful bispilocarpic acid ester derivatives of general formula (I), wherein Y is -C(=O)-R, wherein R is C1-C4-alkyl, C3-C6-cycloalkyl or phenyl, whereby W is a group of formula (Ia), or Y is a group of formula (Ib), whereby W is R', which is C1-C4-alkyl or C3-C6-cycloalkyl, wherein Y has the meaning given above, and A is a direct bond or a methylene group, which can be substituted with hydroxy, the group Y-O- wherein Y has the meaning given, or with one or two methyl groups, and B is a direct bond, methylene or ethylene, and their acid addition salts.
摘要翻译：本发明的目的是药学上有用的通式（I）的双壳糖酸酯衍生物，其中Y是-C（= O）-R，其中R是C 1 -C 4烷基，C 3 -C 6环烷基或苯基，由此W 是式（Ia）的基团，或Y是式（Ib）的基团，其中W是R'，它是C1-C4-烷基或C3-C6-环烷基，其中Y具有上面给出的含义，A 是直接键或亚甲基，其可以被羟基取代，YO-基团，其中Y具有给定的含义，或与一个或两个甲基，B是直接键，亚甲基或亚乙基，以及它们的酸加成盐。

5. 发明申请

WO1992011269A1 NOVEL METHYLENEBISPHOSPHONIC ACID DERIVATIVES 审中-公开
标题翻译：新型亚甲基双膦酸衍生物
公开(公告)号：WO1992011269A1
公开(公告)日：1992-07-09
申请号：PCT/FI1991000395
申请日：1991-12-18
申请人： HUHTAMÄKI OY , POHJALA, Esko , HEIKKILÄ-HOIKKA, Marjaana , NIKANDER, Hannu , HANHIJÄRVI, Hannu
发明人： HUHTAMÄKI OY
IPC分类号： C07F09/58
CPC分类号： C07F9/4025 , C07F9/58
摘要： Novel pharmacologically active methylenebisphosphonates having formula (I) wherein R -R independently are C1-C10-alkyl, C3-C10-cycloalkyl, aryl, aralkyl, silyl SiR3 or hydrogen, whereby in formula (I) at least one of the groups R -R is hydrogen and at least one of the groups R -R is different from hydrogen, Q is hydrogen, hydroxyl, halogen, amino NH2, or OR'1, wherein R'1 is C1-C4-alkyl or acyl, Q is the group ( alpha ) wherein Y is a six-membered heterocyclic group, or a carbocyclic aromatic group, X is a bond, O, S or NR''', wherein R''' is hydrogen, lower alkyl, or acyl, n is the integer 0 to 6, and R' and R" are hydrogen or lower alkyl provided that as a ring atom of the ring Y and/or a chain atom of the group X, there is always at least one heteroatom from the group of O, N and S, including the stereoisomers and the salts of the compounds.
摘要翻译：具有式（I）的新的药理活性亚甲基双膦酸酯，其中R 1 -R 4独立地是C 1 -C 10 - 烷基，C 3 -C 10 - 环烷基，芳基，芳烷基，甲硅烷基SiR 3或氢，其中式（I）至少基团R 1 -R 4之一是氢，并且基团R 1 -R 4中的至少一个不同于氢，Q 1是氢，羟基，卤素，氨基NH 2，或OR 1，其中R 1是C 1 -C 4烷基或酰基，Q 2是其中Y是六元杂环基或碳环芳基，X是键，O ，S或NR“'，其中R”'是氢，低级烷基或酰基，n是整数0至6，并且R'和R“是氢或低级烷基，条件是作为环的环原子 Y和/或X基团的链原子，总是存在至少一个来自O，N和S基团的杂原子，包括立体异构体和化合物的盐。

6. 发明申请

WO1995000144A1 COMPOSITION FOR OPHTHALMIC USE 审中-公开
标题翻译：眼用组合物
公开(公告)号：WO1995000144A1
公开(公告)日：1995-01-05
申请号：PCT/FI1994000270
申请日：1994-06-17
申请人： LEIRAS OY , URTTI, Arto , JÄRVINEN, Tomi , SUHONEN, Pekka , LEHMUSSAARI, Kari , REUNAMÄKI, Timo , ALARANTA, Sakari , OKSALA, Olli , POHJALA, Esko , HANHIJÄRVI, Hannu
发明人： LEIRAS OY
IPC分类号： A61K31/415
CPC分类号： B82Y5/00 , A61K9/0048 , A61K31/415 , A61K47/40 , A61K47/6951
摘要： The present invention relates to a composition for the topical administration of bispilocarpic acid diesters to the eye in the form of an aqueous solution, which includes cyclodextrin and optionally a viscosity and enhancing and pH-adjusting agent.
摘要翻译：本发明涉及一种以水溶液形式向眼睛局部施用双糖皮质二酯的组合物，其包括环糊精和任选的粘度和增强和pH调节剂。

7. 发明申请

WO1992011268A1 NOVEL METHYLENEBISPHOSPHONIC ACID DERIVATIVES 审中-公开
标题翻译：新型亚甲基双膦酸衍生物
公开(公告)号：WO1992011268A1
公开(公告)日：1992-07-09
申请号：PCT/FI1991000396
申请日：1991-12-18
申请人： HUHTAMÄKI OY , HANHIJÄRVI, Hannu , NUPPONEN, Heikki , VEPSÄLÄINEN, Jouko , POHJALA, Esko
发明人： HUHTAMÄKI OY
IPC分类号： C07F09/44
CPC分类号： C07F9/6533 , C07F9/4423
摘要： The invention relates to novel methylenebisphosphonic acid ester amide derivatives of general formula (I), in which formula W , W , W and W are independently the group OR or the group NR R wherein R , R and R independently are hydrogen or straight or branched, optionally unsaturated C1-C22-alkyl, optionally substituted, optionally unsaturated C3-C10-cycloalkyl, aryl, aralkyl or silyl SiR3, or the groups R and R form together with the adjacent nitrogen atom a 3 to 10-membered saturated, partly saturated or aromatic heterocyclic ring, wherein in addition to the nitrogen atom, there may be one or two heteroatoms from the group N, O and S, provided that in formula (I) at least one of the groups W , W , W and W is hydroxy and at least one of the groups W , W , W and W is the amino group NR R , Q and Q are independently hydrogen, fluorine, chlorine, bromine or iodine, including the stereoisomers, such as the geometrical isomers and the optically active isomers, of the compounds, as well as the pharmacologically acceptable salts of the compounds.
摘要翻译：本发明涉及通式（I）的新型亚甲基双膦酸酯酰胺衍生物，其中式W 1，W 2，W 3和W 4独立地为OR 1或基团 NR 2 R 3其中R 1，R 2和R 3独立地是氢或直链或支链的，任选不饱和的C 1 -C 22 - 烷基，任选取代的，任选不饱和的C 3 -C 10 - 环烷基，芳基，芳烷基或甲硅烷基SiR 3，或基团R 2和R 3与相邻的氮原子一起形成3至10元饱和，部分饱和或芳族杂环，其中除了氮原子外，还有可以是来自基团N，O和S的一个或两个杂原子，条件是在式（I）中，基团W 1，W 2，W 3和W 4中的至少一个是羟基，基团W 1，W 2，W 3和W 4中的至少一个是氨基NR 2 R 3，Q 1和Q 2独立地是氢，氟，氯，溴或碘，包括立体异构体，如几何异构体 d化合物的旋光异构体，以及化合物的药理学上可接受的盐。

8. 发明申请

WO1992009583A1 NOVEL PILOCARPINE DERIVATIVES AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：新型吡啶衍生物及其制备方法
公开(公告)号：WO1992009583A1
公开(公告)日：1992-06-11
申请号：PCT/FI1991000359
申请日：1991-11-27
申请人： HUHTAMÄKI OY , JÄRVINEN, Tomi , PEURA, Pekka , SUHONEN, Pekka , URTTI, Arto , HANHIJÄRVI, Hannu , POHJALA, Esko
发明人： HUHTAMÄKI OY
IPC分类号： C07D233/64
CPC分类号： C07D233/64 , C07D405/14
摘要： The object of the invention are novel bispilocarpates useful in the treatment of glaucoma and having general formula (I), wherein A) Y is hydrogen or the acyl group (II), and W is the group -O-A-O-Z-Y', wherein Y' is hydrogen or the acyl group (III), the groups R and R' having different meanings and may be the same or different and A is an aliphatic or aromatic bridging group, and -Z-Y' is (IV), or B) W is OR, wherein R has the same meaning as above, Y is (V), where R' has the same meaning as above, B means the same as A and Z'-OR' is (VI) or C) W and Y together mean -A-O-Z-C-B-C-, where the symbols have the same meanings as above.
摘要翻译：本发明的目的是用于治疗青光眼并具有通式（I）的新颖双胶囊，其中A）Y是氢或酰基（II），W是基团-OAOZ-Y'，其中Y' 是氢或酰基（III），基团R和R'具有不同的含义并且可以相同或不同，A是脂族或芳族桥连基团，-ZY'是（Ⅳ）或B）W是 OR，其中R具有与上述相同的含义，Y为（V），其中R'具有与上述相同的含义，B表示与A相同，Z'-OR'为（VI）或C）W和Y一起平均值-AOZCBC-，其符号具有与上述相同的含义。

9. 发明申请

WO1995026712A1 OPHTHALMIC COMPOSITION CONTAINING AN ION SENSITIVE, HYDROPHILIC POLYMER AND AN INORGANIC SALT IN A RATIO WHICH GIVES LOW VISCOSITY 审中-公开
标题翻译：含有敏感性的亲水性组合物，水解聚合物和无机盐在低粘度的比例
公开(公告)号：WO1995026712A1
公开(公告)日：1995-10-12
申请号：PCT/FI1995000167
申请日：1995-03-29
申请人： LEIRAS OY , LEHMUSSAARI, Kari , VARTIAINEN, Eija , REUNAMÄKI, Timo , OKSALA, Olli , ALARANTA, Sakari , POHJALA, Esko
发明人： LEIRAS OY
IPC分类号： A61K09/00
CPC分类号： A61K9/0048 , A61K47/32 , Y10S514/912
摘要： The present invention is directed to an ophthalmic composition in the form of a topical aqueous solution consisting essentially of: an ophthalmologically active agent containing basic groups, an ion sensitive, hydrophilic polymer containing acidic groups in an amount of 0.004 to 1.5 % by weight, at least one salt selected from the group of inorganic salts and buffers in a total amount of from 0.01 to 2.0 % by weight, and optionally a wetting agent and a preservative, the ratio between salt and polymer being such that the solution exhibits a viscosity of less than 1000 mPas, and the pH of the solution is 4.0 to 8.0. The composition contains a sufficient amount of polymer to provide for a controlled absorption of the drug into the eye, its viscosity having been reduced to provide for better handling characteristics.
摘要翻译：本发明涉及一种局部水溶液形式的眼用组合物，其基本上由以下组成：含有碱性基团的眼科活性剂，含有0.004至1.5重量％的酸性基团的离子敏感的亲水性聚合物，选自无机盐和缓冲剂组中的至少一种盐，其总量为0.01至2.0重量％，以及任选的润湿剂和防腐剂，盐和聚合物之间的比例使得溶液表现出较小的粘度超过1000mPas，溶液的pH为4.0〜8.0。组合物含有足够量的聚合物以提供药物对眼睛的受控吸收，其粘度已经降低以提供更好的处理特性。

10. 发明申请

WO1995013054A1 PROCESS FOR PREPARING A CLODRONATE PREPARATION 审中-公开
标题翻译：制备氯仿制剂的方法
公开(公告)号：WO1995013054A1
公开(公告)日：1995-05-18
申请号：PCT/FI1994000509
申请日：1994-11-11
申请人： LEIRAS OY , POHJALA, Esko , NUPPONEN, Heikki , LEHMUSSAARI, Kari
发明人： LEIRAS OY
IPC分类号： A61K09/16
CPC分类号： A61K31/663 , A61K9/0095 , A61K9/1688 , A61K9/2054 , A61K9/4858 , A61K9/5042 , A61K31/66
摘要： The object of the invention is a process for preparing a clodronate preparation which process is characterized in that clodronate is crystallized as disodium clodronate tetrahydrate from an aqueous solution of disodium clodronate; the resulting disodium clodronate tetrahydrate is dry granulated by compressing in such a way that the crystal structure of the disodium clodronate tetrahydrate is preserved and by crumbling and screening the mass to granules of a suitable size; the dry granulated disodium clodronate tetrahydrate is optionally mixed with suitable excipients, such as filling agents and gliding agents and, if necessary, disintegrants.
摘要翻译：本发明的目的是制备氯膦酸盐制剂的方法，该方法的特征在于氯膦酸盐从氯代膦酸二钠的水溶液中结晶为氯四膦酸二钠四水合物; 所得到的氯四膦酸四水合物二钠通过压缩干燥造粒，使得氯二膦酸二钠四水合物的晶体结构得以保存，并且将物质粉碎并筛分成适合尺寸的颗粒; 任选地将干粒状氯膦酸二钠四水合物与合适的赋形剂混合，例如填充剂和滑动剂，如果需要，与崩解剂混合。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式